Evaluation of Some Mannich Bases Derived from Substituted Acetophenones Against P-388 Lymphocytic Leukemia and on Respiration in Isolated Rat Liver Mitochondria
作者:J.R. Dimmock、K. Shyam、N.W. Hamon、B.M. Logan、S.K. Raghavan、D.J. Harwood、P.J. Smith
DOI:10.1002/jps.2600720812
日期:1983.8
Series of 3-dimethylamino-1-aryl-1-propanone hydrobromides (IV) and 3-dimethylamino-2-dimethylaminomethyl-1-aryl-1-propanone dihydrobromides (V) were synthesized. Evaluation of these derivatives against P-388 lymphocytic leukemia growth revealed that two compounds show promise as antineoplastic agents. Compounds of the V series were unstable in phosphate buffer (in contrast to series IV), and when
合成了一系列的3-二甲基氨基-1-芳基-1-丙酮氢溴酸盐(IV)和3-二甲基氨基-2-二甲基氨基甲基-1-芳基-1-丙酮二氢溴酸盐(V)。这些衍生物对P-388淋巴细胞白血病生长的评估表明,两种化合物显示出作为抗肿瘤药的希望。V系列化合物在磷酸盐缓冲液中不稳定(与IV系列相反),并且当两个系列化合物中都存在相同的核取代基时,V在刺激和抑制呼吸道呼吸方面比IV活性高约100倍。从大鼠肝细胞分离出的线粒体。这两个系列的代表均表明,线粒体的呼吸受水性缓冲液pH值从7.4更改为6.9或6.4以及温度从37度降低到20度的影响。